1. Stem Cell/Wnt
  2. β-catenin
  3. Tegatrabetan

Tegatrabetan (Synonyms: BC2059)

Cat. No.: HY-109103 Purity: 96.40%
Handling Instructions

Tegatrabetan (BC2059) is a β-Catenin antagonist. Tegatrabetan disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1).

For research use only. We do not sell to patients.

Tegatrabetan Chemical Structure

Tegatrabetan Chemical Structure

CAS No. : 1227637-23-1

Size Price Stock Quantity
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 430 In-stock
Estimated Time of Arrival: December 31
100 mg USD 730 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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Description

Tegatrabetan (BC2059) is a β-Catenin antagonist. Tegatrabetan disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1)[1].

IC50 & Target

β-Catenin[1]

In Vitro

Tegatrabetan (BC2059; 20-100 nM; 48 hours) inhibits cell proliferation in suspension culture over 120 hours and induces apoptosis of cultured human acute myeloid leukemia (AML) HL-60, OCI-AML3 and MV4-11 cells dose-dependently[1].
Tegatrabetan (20 and 50 nM; 24 hours) induces a modest but significant accumulation of cells in the G0/G1 phase, with a concomitant decline in the G2/M phase of the cell cycle[1].
Tegatrabetan (100 nM, 24 hours) depletes the levels of β-catenin and its target genes, including c-MYC and survivin without affecting the levels of the TBL1 in OCI-AML3, HL-60 and MV4-11 cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: HL-60, OCI-AML3 and MV4-11 cells
Concentration: 20, 50, and 100 nM
Incubation Time: 48 hours
Result: Dose-dependently inhibited cell proliferation.

Cell Cycle Analysis[1]

Cell Line: OCI-AML3 cells
Concentration: 20 and 50 nM
Incubation Time: 24 hours
Result: Dose-dependently induced cell cycle growth arrest.

Western Blot Analysis[1]

Cell Line: OCI-AML3, HL-60 and MV4-11 cells
Concentration: 100 nM
Incubation Time: 24 hours
Result: Treatment depleted β-Catenin expression levels.
In Vivo

Tegatrabetan (BC2059; 1.0 or 5.0 mg/kg/day; intravenously) significantly improves the median survival of the mice from approximately 17.5 to 39 days. Treatment with Tegatrabetan (10 mg/kg/day; intravenously) alone further improves the median survival to 51.5 days[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NOD/SCID mice bearing OCI-AML3 xenografts[1]
Dosage: 1 mg/kg; 5 mg/kg; 10 mg/kg
Administration: Intravenously; 1 mg/kg daily 4 days per week or 5 mg/kg or 10 mg/kg of BC2059 twice per week (Tuesday and Thursday) for 3 weeks.
Result: Treatment significantly improved survival of NOD/SCID mice bearing OCI-AML3 xenografts.
Molecular Weight

588.74

Formula

C₂₈H₃₆N₄O₆S₂

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (212.32 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6985 mL 8.4927 mL 16.9854 mL
5 mM 0.3397 mL 1.6985 mL 3.3971 mL
10 mM 0.1699 mL 0.8493 mL 1.6985 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (4.25 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (4.25 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 98.19%

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Tegatrabetan
Cat. No.:
HY-109103
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